Remibrutinib (LOU064) - 10mM in DMSO, high purity , CAS No.1787294-07-8

Item Number

R422177

• Synonyms: Remibrutinib (LOU064) | GTPL10457 | N-(3-(6-Amino-5-(2-(N-methylacrylamido)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide | N-[3-[6-Amino-5-[2-[methyl(1-oxo-2-propen-1-yl)amino]ethoxy]-4-pyrimidinyl]-5-fluoro-2-methylpheny
• Specifications & Purity: Moligand™, 10mM in DMSO
• Biochemical and Physiological Mechanisms: Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™

Product Description

Information

Remibrutinib (LOU064) Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.

Targets

BTK (Cell-free assay); IL-8 (Cell-free assay); CD69 (Cell-free assay) 1.3 nM; 2.5 nM; 18 nM

In vitro

LOU064 exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for a best-in-class covalent BTK inhibitor for the treatment of autoimmune diseases.

In vivo

LOU064 demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis.

Cell Research(from reference)

Cell lines：human monocytic cell line THP1, Human Blood B cell and Basophil. 

Concentrations：3 nM, 10 nM, 30 nM, 100 nM, 300 nM 

Incubation Time：25 min, 50 min, 75 min, 100 min